• Title/Summary/Keyword: Synthetic drugs

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Effects of Protein Kinase Inhibitors on Gene Activation of Early Embryos in Mouse (생쥐 초기배아의 유전자 활성에 미치는 Protein Kinase Inhibitors의 영향)

  • Lee, Jeong-Eun;Chai, Young-Gyu;Bae, In-Ha;Yoon, Young-Dal;Kim, Moon-Kyoo
    • Clinical and Experimental Reproductive Medicine
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    • v.22 no.2
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    • pp.191-201
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    • 1995
  • Transcriptional activation of the embryonic genome initiates at 2-cell stage in mouse embryo and is characterized by the synthesis of TRC which is restricted to 2-cell stage. To investigate the roles of various protein kinases on the embryonic gene activation, the effects of protein kinase inhibitors on in vitro development and protein synthetic profiles of the early mouse embryos were examinded. None of ${\alpna}-amanitin$ which is a mRNA synthetic inhibitor, H8 which is a PKA inhibitor, and H7 which is a PKC inhibitor, affected on first cleavage of mouse 1-cell embryos in vitro. However, all of these drugs inhibited the second cleavage. When the drugs were removed following treatment for 6 hours, H8 or H7 treatment showed little inhibition on subsequent development of 1-cell embryos to 2-cell stage or further. In contrast, ${\alpna}-amanitin$ irreversibly inhibited the development of 1-cell embryos to 2-cell stage following removal of the drug. Genistein, a TPK inhibitor, inhibited both the first cleavage of 1-cell embryos and the second cleavage of 2-cell embryos, suggesting that TPK activity may be important during the early cleavages. All of the above four drugs inhibited TRC synthesis as shown by the fluorographic analysis of $[^{35}S]-Met$ labeled protein profiles. When late 1-cell embryos were treated with H7 and analyzed synthetic patterns of $[^{35}S]-Met$ labeled protein, the quantitative differences of protein synthesis on SDS-PAGE appeared on 77 kD and 33 kD region at $32{\sim}38$ hours post hCG. From these studies, transcriptional activation of embryonic genome is not essenting to the mouse 1-cell embryos to develop to 2-cell stage. Hawever, TPK activity is reguisite for both the first cleavage and second cleavage. Similarly, both PKC and PKA activities are required for the second cleavage of mouse embryos, but not for the first cleavage.

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Synthesis of unnatural compounds by enzyme engineering

  • Morita, Hiroyuki
    • Proceedings of the Plant Resources Society of Korea Conference
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    • 2019.04a
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    • pp.34-34
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    • 2019
  • About 60% of the present drugs were developed from natural products with unique chemical diversity and biological activities. Hence, discovery of new bioactive compounds from natural products is still important for the drug development. On the other hand, breakthrough made in synthetic biology has also begun to supply us with many useful compounds through manipulation of biosynthetic gene for secondary metabolites. Theoretically, this approach can also be exploited to generate new unnatural compounds by intermixing genes from different biosynthetic pathway. Considering the potential, we are studying about bioactive compounds in natural sources, as well as the biosynthesis of natural products including engineering of the secondary metabolite enzymes to make new compounds in order to construct the methodological basis of the synthetic biology. In this symposium, engineering of secondary metabolite enzymes that are involved in the biosynthesis of plant polyketides to generate new compounds in our laboratory will be mainly introduced.

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Design, Synthesis and Biological Activities of Novel Vanilloid Receptor Antagonists

  • Lee, Bo-Young;Suh, Young-Ger;Lee, Yong-Sil;Min, Kyung-Hoon;Kim, Jin-Kwan;Seung, Ho-Sun;Park, Young-Ho
    • Proceedings of the PSK Conference
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    • 2003.04a
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    • pp.244.1-244.1
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    • 2003
  • Advances in understanding of pain and analgesia have been made. Over the past few years, we have designed and synthesized a series of VR agonists, based on the structures of 12-HPETE and capsaicin. the natural VR agonist. But for the development of analgesic drugs, these synthetic VR agonists had problems like burning sensation. hypothermia. etc. So our recent studoes have focused on designs and syntheses of VR antagonists based on the structure of capsaicin(natural VR agonist), and capsazepine(synthetic VR antagonist). (omitted)

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Application of Bioisosterism in Development of Novel Cardiotonics Based on (2'-Aminoethyl)carbostyril and (2'-Aminoethyl)-1-hydroxy-2-pyridone Systems

  • Yoon, Sung-Hwa
    • Journal of Pharmaceutical Investigation
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    • v.22 no.3
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    • pp.49-63
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    • 1992
  • Two different types of chemical manipulations of dobutamine were investigated in order to develop novel, improved cardiotonic drugs. Three new analogues of carbostyril, in which the m-hydroxy group of dobutamine was isosterically modified with an amide type carbostyril system, were synthesized from, ${\rho}-methoxyphenethylamine$ via multi-steps. Two analogues of (2'-aminoethyl)-1-hydroxy-2-pyridone system which has isosteric structural similarity with dopamine without having the COMT vulnerable m-hydroxy group were synthesized via 12 synthetic steps. Their biological stabilities in various media and inotropic activities were evaluated.

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Novel Asymmetric Synthesis of Unsaturated 1,2-Amino Alcohols

  • Kim, Ji-Duck;Jung, Young-Hoon
    • Proceedings of the PSK Conference
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    • 2002.10a
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    • pp.231.2-232
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    • 2002
  • The synthesis of chiral 1,2-amino alcohols has been an area of intense study in the synthetic and industrial fields, because of their important roles in organic synthesis as fundamental building blocks and their occurrence in a number of natural products. drugs. and chiral auxiliaries or ligands. General methods for the synthesis of these compounds can be divided into two large categories: functional group transformations and the C-C or the C-N bond formations. (omitted)

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Chemometric Tool of Chromatographic Pattern Recognition for the Analysis of Complex Mixtures

  • Park, Man-Ki;Park, Jeong-Hill;Cho, Jung-Hwan;Kim, Na-Young;Kang, Jong-Seong
    • Archives of Pharmacal Research
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    • v.15 no.4
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    • pp.376-378
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    • 1992
  • A chemical tool was developed for the analysis of complex mixtures such as crude drugs by the method of pattern recognition. Pattern recognition was accomplished by a multiple reference peak identification method and three kinds of outlier statistics. This tool was tested on the analysis of synthetic mixtures.

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Aspirin (I) Discovery, Current and Potential New Therapeutic Uses, and Mechanism of Action

  • Kim, Dong-Han
    • Archives of Pharmacal Research
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    • v.1 no.1
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    • pp.41-54
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    • 1978
  • Aspirin is one of the oldest synthetic drugs and remains the most widely used medical agent. It is a household remedy effective in treating such common ailments as headache, minor muscular pain and fever. Aspirin is the drug choice for rheumatic fever and arthritis which some five million Americans suffer. Lately it has been established by double-blind and randomized clinical studies that regular aspirin intake reduces the incidence of mild strokes and heart attackes.

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Development of Synthetic Drugs Management Applications Using Smartphone (스마트폰을 이용한 합성 의약품 관리 어플리케이션 개발)

  • Han, Jin-Hyung;Seo, HongJu;Lee, HwaMin
    • Proceedings of the Korea Information Processing Society Conference
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    • 2013.11a
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    • pp.445-448
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    • 2013
  • 본 논문에서는 어플리케이션을 통하여 우리가 자주 사용하는 의학품을 좀 더 안전하고 편리하게 다루어 사용자가 무분별하게 사용하는 약물 오남용을 줄이고 안전사고를 예방하는데 초점을 두었다. 또한 어플리케이션 특유의 편리함과 간편함을 통하여 사용자에게 좀 더 다가가는데 목적을 두었다.

Management of Veterinary Drug Residues in Food (식품 중 잔류동물용의약품의 안전관리)

  • Oh, Jae-Ho;Kwon, Chan-Hyeok;Jeon, Jong-Sup;Choi, Dong-Mi
    • Korean Journal of Environmental Agriculture
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    • v.28 no.3
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    • pp.310-325
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    • 2009
  • Veterinary drugs have been used to prevent livestock diseases for many years. In spite of having advantages, sometimes indiscriminate application, overdose and abuse may cause risk for human. Therefore, management and risk assessment of veterinary drugs become essential to ensure food safety. So the National Veterinary Research & Quarantine Service (NVRQS) impose on registration for use of veterinary drugs also Korea Food and Drug Administration (KFDA) fixed the maximum residue limits (MRLs) for veterinary drugs in food. Basically, KFDA set MRLs based on the veterinary drugs residual data. Moreover, KFDA estimates the theoretical maximum daily intake (TMDI) with food consumption data and population mean body weight. Recently, 116 veterinary drug MRLs including banned veterinary drugs have been established and other 32 veterinary drugs MRLs will be established within 2009. In 2010, MRLs among antibiotics and synthetic antibacterial agents in livestock fishery products (including milk and eggs) and honey (including royal jelly and propolis) which have not been set in Korea Food Code and Codex Alimentarius Commission (CAC) will be regulated as uniform limit (0.03 mg/kg). In future, veterinary drugs will be controlled strictly to strengthen public health by improving analytical method.

Alternative drug therapies are superior to epidermal growth factor receptor -targeted chemotherapeutic drug responses in non-small cell lung cancer

  • Sikdar, Sourav;Khuda-Bukhsh, Anisur Rahman
    • CELLMED
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    • v.3 no.2
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    • pp.10.1-10.8
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    • 2013
  • Cancer is one of the major dreaded diseases causing high mortality. Lung cancer is second in position of all cancer related deaths and mainly divided into two morphologic sub-types: small-cell lung cancer and non-small cell lung cancer (NSCLC). NSCLC is an aggressive neoplasm which hardly responds to any conventional chemotherapy. Epidermal growth factor receptor (EGFR) belongs to the ErbB family of receptor tyrosine kinase that is mainly over-expressed in NSCLC. EGFR is mainly involved in the pathogenesis and progression of different carcinoma. In vivo and in vitro studies suggest that EGFR and EGF like peptides are often over-expressed in human NSCLC and these proteins are able to induce cell transformation. The conventional therapies mostly inhibit the EGFR activity and expression level in human NSCLC with the use of some EGFR-inhibitors like HKI-272, EKB569, CL-387785 etc. and some synthetic chemotherapeutic drugs like erlotinib, gefitinib, plumbagin, docetaxel, cisplatin etc., alone or in combination of two or more drugs. These therapies selectively act by competitive inhibition of the binding of adenosine triphosphate to the tyrosine kinase domain of the EGFR, resulting in inhibition of the EGFR signaling pathway. But these chemotherapeutic drugs have some cytotoxic activities to the normal cells and have some adverse side-effects. Recent studies on some traditional alternative therapies including some herbal and plant extracts, active ingredients like curcumin, different homeopathic drugs, etc. can target EGFR-signalling in NSCLC with less toxic side-effects are being currently developed.